Interaction potential of the endothelin

• Verfasst von: Weiß, Johanna [VerfasserIn]
• Verfasst von: Haefeli, Walter E. [VerfasserIn]
• Titel: Interaction potential of the endothelin
• Titelzusatz: a receptor antagonist atrasentan with drug transporters and drug-metabolising enzymes assessed in vitro
• Verf.angabe: Johanna Weiss, Walter Emil Haefeli
• E-Jahr: 2011
• Jahr: 31 July 2011
• Umfang: 6 S.
• Fussnoten: Gesehen am 18.11.2022
• Titel Quelle: Enthalten in: Cancer chemotherapy and pharmacology
• Ort Quelle: Berlin : Springer, 1978
• Jahr Quelle: 2011
• Band/Heft Quelle: 68(2011), 4, Seite 1093-1098
• ISSN Quelle: 1432-0843
• DOI: doi:10.1007/s00280-011-1715-8
• Datenträger: Online-Ressource
• Sprache: eng
• Sach-SW: Atrasentan
• Sach-SW: CYPs
• Sach-SW: Drug transporters
• Sach-SW: Drug-drug interaction
• Sach-SW: Endothelin receptor A antagonist
• Sach-SW: Induction
• K10plus-PPN: 1822873096

Abstract

Atrasentan is a highly potent and selective endothelin receptor A (ETA) antagonist under development for the treatment of prostate cancer. Only little data exist on its interaction with drug-metabolising enzymes and drug transporters possibly influencing its safety and effectiveness. Our study evaluated whether atrasentan can induce the expression of relevant human drug transporters and cytochrome P450 isozymes (CYPs), whether it retains its efficiency in multidrug resistant cell lines, and whether it inhibits P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP).